Benzodiazepines: Drugs with Chemical Skeletons Suitable for the Preparation of Metallacycles with Potential Pharmacological Activity

The synthesis of organometallic compounds with potential pharmacological activity has attracted the attention of many research groups, aiming to take advantage of aspects that the presence of the metal-carbon bond can bring to the design of new pharmaceutical drugs. In this context, we have gathered studies reported in the literature in which psychoactive benzodiazepine drugs were used as ligands in the preparation of organometallic and metal complexes and provide details on some of their biological effects. We also highlight that most commonly known benzodiazepine-based drugs display molecular features that allow the preparation of metallacycles via C-H activation. These organometallic compounds merit further attention regarding their potential biological effects, not only in terms of psychoactive drugs but also in the search for drug replacements, for example, for cancer treatments.

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Pharmaceutical drugs and other substances with pharmacological activity in the environment: a threat to biodiversity?

Conservation Science ◽

10.3126/cs.v2i1.13764 ◽

2015 ◽

Vol 2 (1) ◽

pp. 12-16 ◽

Cited By ~ 3

Author(s):

Bruno Nunes

Keyword(s):

Environmental Exposure ◽

Pharmacological Activity ◽

Selective Pressure ◽

Pharmaceutical Drugs ◽

Human Origin ◽

The Future ◽

Other Substances

Drugs of human origin are now dispersed in all ecosystems, and non-target exposed biota are likely to be impacted in the future by a large number of substances with unpredictable consequences. One of the potential effects of drugs (and other substances with pharmacological activity) is the exertion of selective pressure, favouring an artificial process of selection, in which sensitive organisms may be favoured. We bring to discussion the consequences expected from chronic environmental exposure of biota to two major classes of chemicals that are nowadays released thoroughly into the environment: stimulants and neuroendocrine drugs.Conservation Science Vol.2(1) 2014: 12-16

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RECENTES APLICAÇÕES DO ORGANOFOTOCATALISADOR 1,2,3,5-TETRAQUIS(CARBAZOL-9-IL)-4,6- DICIANOBENZENO EM TRANSFORMAÇÕES QUÍMICAS

Química Nova ◽

10.21577/0100-4042.20170674 ◽

2020 ◽

Author(s):

Lucas Pugnal ◽

Emanuele Pissinati ◽

Karina Quaglio ◽

Márcio Paixão

Keyword(s):

Transition Metal ◽

Metal Complexes ◽

Transition Metal Complexes ◽

Chemical Transformations ◽

Redox Potentials ◽

Research Groups ◽

Organic Fluorophores ◽

Metal Free ◽

Polypyridine Complexes ◽

Distinguished Research

RECENT APPLICATIONS OF THE ORGANIC PHOTOCATALYST 1,2,3,5-TETRAKIS(CARBAZOL-9-YL)- 4,6-DICIANOBENZENE IN CHEMICAL TRANSFORMATIONS. Ruthenium and iridium polypyridine complexes are among the most employed photocatalysts described in literature. The broad applicability is due to the redox potentials and long half-life times of the excited state which these molecules presented. The pursuit for metal-free alternatives has been intensified in the last few years, therefore, many organic fluorophores were successfully employed as photocatalysts. Among them, 1,2,3,5-tetrakis(carbazol-9-yl)- 4,6-dicianobenzene (4CzIPN) recently drawn attention of the community, and it’s been widely employed by distinguished research groups. Recent studies have shown that this catalyst do not only present similar properties to transition metal complexes, but also, its synthesis can be accomplished more easily and less expensive when compared with the metallic photocatalysts above mentioned. Therefore, 4CzIPN constitutes a metal-free alternative to replace transition metal complexes in conventional photochemical protocols. Moreover, it’s as a powerful ally in the development of new photochemical approaches. In this work, we aim to summarize recent applications of 4CzIPN as catalyst in the emerging field of redox photocatalysis.

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Anabolic and antiresorptive actions of locally delivered bisphosphonates for bone repair

Bone and Joint Research ◽

10.1302/2046-3758.710.bjr-2018-0015.r2 ◽

2018 ◽

Vol 7 (10) ◽

pp. 548-560 ◽

Cited By ~ 8

Author(s):

I. Qayoom ◽

D. B. Raina ◽

A. Širka ◽

Š. Tarasevičius ◽

M. Tägil ◽

...

Keyword(s):

Bone Resorption ◽

Bone Regeneration ◽

Bone Morphogenetic Proteins ◽

Bone Repair ◽

Biological Effects ◽

Research Groups ◽

Preclinical Models ◽

Implant Fixation ◽

Local Use

During the last decades, several research groups have used bisphosphonates for local application to counteract secondary bone resorption after bone grafting, to improve implant fixation or to control bone resorption caused by bone morphogenetic proteins (BMPs). We focused on zoledronate (a bisphosphonate) due to its greater antiresorptive potential over other bisphosphonates. Recently, it has become obvious that the carrier is of importance to modulate the concentration and elution profile of the zoledronic acid locally. Incorporating one fifth of the recommended systemic dose of zoledronate with different apatite matrices and types of bone defects has been shown to enhance bone regeneration significantly in vivo. We expect the local delivery of zoledronate to overcome the limitations and side effects associated with systemic usage; however, we need to know more about the bioavailability and the biological effects. The local use of BMP-2 and zoledronate as a combination has a proven additional effect on bone regeneration. This review focuses primarily on the local use of zoledronate alone, or in combination with bone anabolic factors, in various preclinical models mimicking different orthopaedic conditions. Cite this article: I. Qayoom, D. B. Raina, A. Širka, Š. Tarasevičius, M. Tägil, A. Kumar, L. Lidgren. Anabolic and antiresorptive actions of locally delivered bisphosphonates for bone repair: A review. Bone Joint Res 2018;7:548–560. DOI: 10.1302/2046-3758.710.BJR-2018-0015.R2.

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Structural Alerts for Predicting Clastogenic Activity of Pro-oxidant Flavonoid Compounds

CrossRef Listing of Deleted DOIs ◽

10.1177/1087057111421623 ◽

2011 ◽

Vol 17 (2) ◽

pp. 216-224 ◽

Cited By ~ 9

Author(s):

Estela Guardado Yordi ◽

Enrique Molina Pérez ◽

Maria Joao Matos ◽

Eugenio Uriarte Villares

Keyword(s):

Molecular Design ◽

Biological Effects ◽

Screening Method ◽

Automatic Generation ◽

Quantitative Structure Activity Relationship ◽

Hydroxyl Group ◽

Hydroxyl Groups ◽

Qsar Study ◽

Molecular Features ◽

Structural Alerts

Flavonoids have been reported to exert multiple biological effects that include acting as pro-oxidants at very high doses. The authors determined a structural alert to identify the clastogenic activity of a series of flavonoids with pro-oxidant activity. The methodology was based on a quantitative structure–activity relationship (QSAR) study. Specifically, the authors developed a virtual screening method for a clastogenic model using the topological substructural molecular design (TOPS-MODE) approach. It represents a useful platform for the automatic generation of structural alerts, based on the calculation of spectral moments of molecular bond matrices appropriately weighted, taking into account the hydrophobic, electronic, and steric molecular features. Therefore, it was possible to establish the structural criteria for maximal clastogenicity of pro-oxidant flavonoids: the presence of a 3-hydroxyl group and a 4-carbonyl group in ring C, the maximal number of hydroxyl groups in ring B, the presence of methoxyl and phenyl groups, the absence of a 2,3-double bond in ring C, and the presence of 5,7 hydroxyl groups in ring A. The presented clastogenic model may be useful for screening new pro-oxidant compounds. This alert could help in the design of new and efficient flavonoids, which could be used as bioactive compounds in nutraceuticals and functional food.

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Molecular On-Surface Synthesis: Metal Complexes, Organic Molecules, and Organometallic Compounds

Advances in Atom and Single Molecule Machines - On-Surface Synthesis ◽

10.1007/978-3-319-26600-8_7 ◽

2016 ◽

pp. 131-165 ◽

Cited By ~ 1

Author(s):

J. Michael Gottfried

Keyword(s):

Metal Complexes ◽

Organic Molecules ◽

Organometallic Compounds

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Application of high pressure spectroscopy to the study of interactions of small gaseous molecules with transition metal complexes and organometallic compounds II. Interaction of vanadium(II) and molybdenum(II) phosphine complexes with CO

Journal of Organometallic Chemistry ◽

10.1016/s0022-328x(00)88976-7 ◽

1981 ◽

Vol 209 (1) ◽

pp. 69-76 ◽

Cited By ~ 10

Author(s):

Victor M. Hall ◽

C. David Schmulbach ◽

William N. Soby

Keyword(s):

High Pressure ◽

Transition Metal ◽

Metal Complexes ◽

Transition Metal Complexes ◽

Organometallic Compounds ◽

Phosphine Complexes

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Synthesis and Characterization of Some Metal Complexes of 4,5-Diazafluoren-9-one and their Biological Effects on Human Carcinoma Cells

Australian Journal of Chemistry ◽

10.1071/ch08342 ◽

2008 ◽

Vol 61 (12) ◽

pp. 975 ◽

Cited By ~ 6

Author(s):

Guo-Liang Lu ◽

Cheuk-Lam Ho ◽

Qiwei Wang ◽

Wai-Yeung Wong ◽

Chung-Hin Chui ◽

...

Keyword(s):

Metal Complexes ◽

Cell Lines ◽

Cancer Cell ◽

Human Cancer ◽

Biological Effects ◽

Cancer Cell Lines ◽

Inhibitory Effect ◽

Ambient Conditions ◽

Human Carcinoma ◽

Human Cancer Cell Lines

Three new transition metal complexes of 4,5-diazafluoren-9-one, [(DAFO)PdCl2], [(DAFO)PtCl2], and [(DAFO)ZnCl2], were prepared in good yields by the reactions between appropriate metal chloride precursors and 4,5-diazafluoren-9-one under ambient conditions. The structures of these metal complexes were established by spectroscopic (Fourier-transform IR, NMR, and fast-atom bombardment mass spectrometry) techniques. The possible biological activity of these compounds on three human cancer cell lines including Hep3B, MDAMB-231, and SKHep-1 was investigated. The results obtained showed that both zinc- and platinum-containing compounds exhibit a similar growth inhibitory effect on these three cancer cell lines when compared with the prototypical cis-platin. In contrast, the corresponding palladium congener is virtually biologically inactive in these trials.

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